产品说明书
CX-5461
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同义名 : | Pidnarulex |
| CAS号 : | 1138549-36-6 | |
| 货号 : | A121589 | |
| 分子式 : | C27H27N7O2S | |
| 纯度 : | 99%+ | |
| 分子量 : | 513.614 | |
| MDL号 : | MFCD21609261 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
H2O: 55 mg/mL(107.08 mM)，配合低频超声，并调节pH至2 |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Deregulated ribosomal RNA synthesis is associated with uncontrolled cancer cell proliferation. RNA polymerase (Pol) I, the multiprotein complex that synthesizes rRNA, is activated widely in cancer. CX-5461, a potent small-molecule inhibitor of rRNA synthesis in cancer cells, selectively inhibits Pol I with IC50 value of 142 nM in the HCT-116 cells. The IC50 for rRNA synthesis for the BJ-hTert normal cell line of 74 nM correlated well with the IC50 values of the solid tumor cell lines (IC50 = 142, 113, and 54 nM, respectively) illustrating that CX-5461 can equivalently inhibit Pol I transcription in cancer and normal cells, but the normal cells can tolerate reductions in rRNA synthesis without induction of cell death. Treatment with 300 nM CX-5461 for 24 hours caused a significant increase from 15% ± 3% to 67% ± 2% in LC3B-II staining (P = 0.0041) in A375 and from 19% ± 2% to 62% ± 3% in LC3B-II staining (P = 0.002) in MIA PaCa-2 cells (LC3B-II, a known marker of autophagy). In addition to autophagy, CX-5461 (300 nM; 24 hours) was able to induce senescence in both cell lines. In two murine xenograft models of human cancers, MIA PaCa-2 and A375, CX-5461 was administered orally (50 mg/kg) either once daily or every 3 days. CX-5461 demonstrated significant MIA PaCa-2 TGI (tumor growth inhibition) equal to 69% on day 31. Likewise, CX-5461 demonstrated significant A375 TGI equal to 79% on day 32[5]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.95mL 0.39mL 0.19mL |
9.73mL 1.95mL 0.97mL |
19.47mL 3.89mL 1.95mL |
| 参考文献 |
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